Discovery of a New Series of 5-HT1A Receptor Agonists

Bioorg Med Chem Lett. 2010 Mar 15;20(6):2017-20. doi: 10.1016/j.bmcl.2010.01.030. Epub 2010 Feb 4.

Abstract

Starting from compounds previously identified as alpha(1)-adrenoceptor antagonists that were also found to bind to the 5-HT(1A) receptor, in an attempt to separate the two activities, a new series of 5-HT(1A) receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT(1A)/alpha(1)=151) and good agonist potency (pD(2)=7.82; E(max)=76), was found to be the most interesting.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Discovery
  • Serotonin 5-HT1 Receptor Agonists*

Substances

  • Serotonin 5-HT1 Receptor Agonists